Synthesis of new benzothiazole derivatives with in-depth In-vitro, In-vivo anti-oxidant, anti-inflammatory and anti-ulcer activities

PLoS One. 2026 Jan 30;21(1):e0337639. doi: 10.1371/journal.pone.0337639. eCollection 2026.

Abstract

Benzothiazoles (BTZ) possess various medicinal benefits and in this study, we have synthesized benzothiazole derivatives by substituting its side chains, and analyzed its spectral analysis along with its antioxidant and anti-inflammatory activity. In-vitro antioxidant activity of the benzothiazole derivatives indicated strong antioxidant potential of 3b, 3d and 3e which were then evaluated for their anti-inflammatory potential in mice's paw edema and ethanol-induced gastric ulcer (GU). The compounds demonstrated strong anti-inflammatory ability in paw edema as well as ethanol-induced gastric ulcer. This was further confirmed by H&E staining and suppressed inflammatory mediators as tumor necrotic factor (TNF-α), nuclear factor B (p-NFkB), and cyclooxygenase-2 (COX-2). The antioxidant ability was assessed by measuring catalase (CAT), glutathione-S-transferase (GST), glutathione (GSH), superoxide dismutase (SOD), and lipid peroxidation (LPO) levels in both edema and ulcer models. Additionally, gastric lesions were detected in the ulcer and low Ulcer index confirmed anti-ulcer ability. These results suggest new benzothiazoles which can be further analyzed through clinical studies.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents* / chemical synthesis
  • Anti-Inflammatory Agents* / chemistry
  • Anti-Inflammatory Agents* / pharmacology
  • Anti-Inflammatory Agents* / therapeutic use
  • Anti-Ulcer Agents* / chemical synthesis
  • Anti-Ulcer Agents* / chemistry
  • Anti-Ulcer Agents* / pharmacology
  • Anti-Ulcer Agents* / therapeutic use
  • Antioxidants* / chemical synthesis
  • Antioxidants* / chemistry
  • Antioxidants* / pharmacology
  • Antioxidants* / therapeutic use
  • Benzothiazoles* / chemical synthesis
  • Benzothiazoles* / chemistry
  • Benzothiazoles* / pharmacology
  • Benzothiazoles* / therapeutic use
  • Catalase / metabolism
  • Cyclooxygenase 2 / metabolism
  • Edema / chemically induced
  • Edema / drug therapy
  • Edema / metabolism
  • Edema / pathology
  • Ethanol
  • Glutathione / metabolism
  • Lipid Peroxidation / drug effects
  • Male
  • Mice
  • Stomach Ulcer* / chemically induced
  • Stomach Ulcer* / drug therapy
  • Stomach Ulcer* / pathology
  • Superoxide Dismutase / metabolism
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Benzothiazoles
  • Antioxidants
  • Anti-Inflammatory Agents
  • Anti-Ulcer Agents
  • Glutathione
  • Tumor Necrosis Factor-alpha
  • Cyclooxygenase 2
  • Ethanol
  • Superoxide Dismutase
  • Catalase